Emulsion Technology for Topical

Nr. 5
LifeScience – Pharma
Biesterfeld Spezialchemie GmbH
Spotlight Emulsion Technology for
Topical Pharmaceutical and Medical Device
Know ...
... How!
Dow Corning®
TI-6021 W/O Formulation Aid
Dow Corning®
Emulsifier 10
Basic Formulation:
Relieving Emulsion (W/Si)
Dow Corning® Emulsifiers:
Water-in-oil (W/O), Water-in-silicone (W/Si) and
Water-in-silicone-and-oil (W/Si-O)
Three criteria are key for topical pharmaceutical and
medical device applications:
● Safety ● Efficacy ● Patient compliance
Emulsions can offer enhanced aesthetics through a
non-greasy and pleasant, smooth feel. Silicone
emulsifiers combining water, silicones and oil allow
to formulate systems with unique properties which
are known to contribute to a higher acceptance by the
patient during long term treatments. Dow Corning has
transferred the well-established technology of silicone
emulsifiers for water-in-oil/silicone and
water-in-silicone-and-oil systems in appropriate
healthcare grade materials:
Dow Corning® Emulsifier 10 and
Dow Corning® TI-6021 W/O Formulation Aid
The requirements for emulsions registered as topical
pharmaceutical or medical device are high. This
means that various requirements must be observed:
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●
●
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●
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Regulatory compliance of ingredients
Emulsion stability
Release of active ingredients
Skin compatibility
Pleasant texture
Cold processing as option to reduce costs and
complexity
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Nr. 5
LifeScience – Pharma
Companion Product
Applications
Consumer Healthcare &
Topical Medical Device
Dow Corning® TI-6021 W/O
Formulation Aid
Pharmaceutical
Applications
Dow Corning® Emulsifier 10
Water-in-silicone and water-in-silicone-and-oil
emulsifier for low viscosity emulsions.
Non-diluted material.
Water-in-oil and water-in silicone-and-oil emulsifier,
very effective at producing water-in-oil emulsions
with a low to medium polarity oil phase.
Can also be used as co-emulsifier in oil-in-watersystems. Non-diluted material.
Low molecular weight ethoxylated silicone surfactant
Alkylmethyl siloxane copolyol
Calculated HLB ~ 4
Calculated HLB ~ 2,2
Formulation Benefits:
• Provides water-in-silicone and water-in-siliconeand-oil emulsions with textures from lotion to cream
• Formulation flexibility with a broad range of
silicones and organic oil phases
• Non-greasy feel
• Low odor
• Cold or hot processing
Formulation Benefits:
• Provides very stable water-in-oil systems without
addition of waxes; up to ~80% of water phase
• Enables water-in-wax emulsions and sticks
• Non-greasy feel
• Rich but “light feel”
• Easy to spread
• Reduces tackiness
• Light skin conditioning properties
• Cold or hot processing
Recommended use-level (RUL):
Allows an addition level as low as 2 %. This addition
level needs to be increased up to 6 % when working
at lower W/Si-Oil ratio.
Recommended use-level (RUL):
2 % for an oil phase ranging from 18-25 % for low
polarity oil and from 25-28 % for medium polarity
oil.
Water/Si+Oil Ratio
80/20
70/30
60/40
Water/Si+Oil Ratio
80/20
70/30
60/40
RUL (%)*
2-3
3-5
5-6
RUL (%)*
1-2
2-4
3-6
Formulation Recommendations:
• Stable emulsions can be prepared by slowly adding
the water phase to the oil phase under mixing;
common mixing devices can be used. The oil phase
should be prepared first by mixing Dow Corning®
TI-6021 W/O Formulation Aid with the selected low
viscosity silicone fluid and/or organic fluid. High
shear mixing at the end of the emulsification process
helps to decrease particle size.
Formulation Recommendations:
• Use of 1 % sodium chloride in the water phase for
formulation stability.
• Consistent, slow addition of the water phase to the
oil phase using a variety of common mixing devices.
Oil phase should be prepared first by mixing
Dow Corning® Emulsifier 10 with selected fluid
(from low to medium polarity). High shear mixing
at the end of the emulsification process will
decrease particle size and build the viscosity.
Regulatory Documentation:
Ingredient Information Package (IIP):
• Ingredient Regulatory Information (IRI)
• Elemental Impurities (EI)
• Summary of Health Data or Opinion Letter
Regulatory Documentation:
• US DMF 16909, European Technical File
• Product Regulatory Information Sheet
• Elemental Impurities (EI)
• Tested for Mutagenicity/Genotoxicity,
Skin Sensitization
*Use levels are simply suggested starting points and will need to be adjusted based on other formulation ingredients.
Nr. 5
LifeScience – Pharma
Formulation process:
Water-in-silicone/oil emulsions
Process to make W/Si-oil emulsion
A: Water Phase
B: Silicone or Oil Phase
Prepare Phase A and B
separately.
Add Water Phase A to
Silicone or Oil Phase B,
very slowly, with low to
medium shear and
speed mixing.
After addition of Phase
B, continue mixing with
same shear but higher
speed mixing.
Emulsion can be completed as such but
in most cases, stability will be improved
by decreasing particle size with high
shear mixing (rotor stator type of
equipment) after emulsification.
Emulsions:
Emulsions are basic dosage forms for topical
pharmaceutical and medical device applications.
They are systems of two immiscible fluids, like
water and oil, where one fluid is finely dispersed
in the other by using an emulsifier. Depending on
which phase forms the droplets you distinguish in
oil-in-water (O/W) or water-in-oil (W/O) emulsions.
W/O, W/Si and W/Si-O systems are emulsions in
which small water droplets are dispersed in the
continuous oil/silicone-phase.
W/Si-O emulsions have gained considerable importance in applications that require the special
properties of silicones – in particular, the excellent
spreading and film-forming properties, e.g.
substantivity, wash-off resistance and a
non-occlusive film. (*1) (*2)
Dow Corning has long term experiences with
W/Si-O emulsifiers which combine performance
with sensory effects. One of the formulators’
biggest challenges is balancing the stability of a
formulation, where the emulsifier level, phase
ratio, silicone/oil phase viscosity and shear/mixing
have to be considered, with aesthetic and
performance parameters. (*1)
Extracted from:
(*1) Cindy Delvallé,
Dow Corning Europe S.A., Belgium, Yasue Kanzaki,
Sayuri Sawayama,
Seiki Tamura,
Dow Corning Co Ltd.; Japan, Rose Bao, Dow Corning
Co.Ltd., China
„Expanding Formulation Possibilities with a
Water-in-oil Silicone Emulsifier
Offering Broad Oil Phase Flexibility“
(*2) Dow Corning Tool Box Tips,
Chemical Manufacturing Solutions,
“Silicone Surfactants: Emulsification”
(*3) Dow Corning Presentation
„Dow Corning Emulsifier Success Kit“
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LifeScience – Pharma
Relieving Emulsion (W/Si)
BSC - Ph.1501
Water in Silicone Emulsion - Non-occlusive
Skin hydration - Skin protection - Excellent sensory feel and smoothness - Reduces tackiness
Phase
Trade Name
Ingredient
A
Deionised Water
Aqua
Emprove®
Urea
Supplier
%
54,0
Merck
8,0
Urea Beads
Sodium Chloride
Sodium Chloride
Saliguard® PG
Phenoxyethanol, Caprylyl
1,0
Salicylates & Chemicals
1,0
Glycol
B
C
1,2 Propanediol
Propylene Glycol
Merck
10,0
Salicylic Acid
Salicylic Acid
Dow Corning® TI-6021
PEG-10 Dimethicone
Dow Corning
4,0
Dow Corning® TI-3021
Dimethicone,
Dow Corning
5,0
Silicone Elastomer Blend
Dimethicone Crosspolymer
Dow Corning® Q7-9120
Dimethicone
Dow Corning
15,0
2,0
W/O Formulation Aid
Silicone Fluid, 20 cSt
100,0
Manufacturing Procedure:
1. Premix phases A, B and C separately.
2. Mix phase B until a clear solution is obtained.
3. Ensure that Silicone Elastomer Blend (Dow Corning® TI-3021) is completely dispersed in phase C.
4. Emulsify slowly phase B to phase C while stirring.
5. Emulsify slowly and stepwise phase A to phase B/C while strong stirring. Homogenize.
Product Features:
Appearance: White emulsion
Viscosity (Brookfield RV: Helipath TF, Speed 10 rpm): Approx. 37.000 mPas
Centrifugation (4.000 rpm, 15 min.): No separation
For further detailed information regarding products, basic formulations or technical details please contact our healthcare team.
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Biesterfeld Spezialchemie GmbH - LifeScience Pharma
Ferdinandstrasse 41
- 20095 Hamburg, Germany
Tel.: +49 40 32008-710 or -252
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healthcare@biesterfeld.com
Registered Office: Hamburg,
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Managing Directors: Dr. Nicole Hamelau, Peter Wilkes
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from the records of our raw material suppliers.
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We shall not be liable for the suitability of the goods for the purpose intended by Customer, unless the achievement of a certain outcome of the utilisation was expressly incorporated into the contract. Our advice, information or recommendations regarding
application shall be provided to the best of our knowledge. As the actual application is
beyond our scope of influence, and as the circumstances of such application are not
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